Reaction Details
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Protein arginine N-methyltransferase 1 [11-371]
Ligand
BDBM178102
Substrate
n/a
Meas. Tech.
PRMT Biochemical Assays
Ki
120±4 nM
IC50
250±15 nM
Citation
Eram, MS; Shen, Y; Szewczyk, MM; Wu, H; Senisterra, G; Li, F; Butler, KV; Kaniskan, Hÿ; Speed, BA; Dela Seña, C; Dong, A; Zeng, H; Schapira, M; Brown, PJ; Arrowsmith, CH; Barsyte-Lovejoy, D; Liu, J; Vedadi, M; Jin, J A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol 11:772-81 (2016) [PubMed] Article More Info.:
Target
Name:
Protein arginine N-methyltransferase 1 [11-371]
Synonyms:
ANM1_HUMAN | HMT2 | HRMT1L2 | IR1B4 | PRMT1 | Protein arginine N-methyltransferase 1 (PRMT1) | Protein arginine methyltransferase 1 (PRMT1) | Protein-arginine N-methyltransferase 1
Type:
Protein
Mol. Mass.:
41506.52
Organism:
Homo sapiens (Human)
Description:
Q99873[11-371]
Residue:
361
Sequence:
MENFVATLANGMSLQPPLEEVSCGQAESSEKPNAEDMTSKDYYFDSYAHFGIHEEMLKDEVRTLTYRNSMFHNRHLFKDKVVLDVGSGTGILCMFAAKAGARKVIGIECSSISDYAVKIVKANKLDHVVTIIKGKVEEVELPVEKVDIIISEWMGYCLFYESMLNTVLYARDKWLAPDGLIFPDRATLYVTAIEDRQYKDYKIHWWENVYGFDMSCIKDVAIKEPLVDVVDPKQLVTNACLIKEVDIYTVKVEDLTFTSPFCLQVKRNDYVHALVAYFNIEFTRCHKRTGFSTSPESPYTHWKQTVFYMEDYLTVKTGEEIFGTIGMRPNAKNNRDLDFTIDLDFKGQLCELSCSTDYRMR
Inhibitor
Name:
BDBM178102
Synonyms:
N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-pyrrol-3-yl)methyl)ethane-1,2-diamine (Compound 2)
Type:
Small organic molecule
Emp. Form.:
C15H18F3N3
Mol. Mass.:
297.3187
SMILES:
CN(CCN)Cc1c[nH]cc1-c1cccc(c1)C(F)(F)F
Structure:
